叶酸修饰的奥沙利铂纳米粒的制备及其体外特性研究

Preparation and in vitro Activity Evaluation of Folate-conjugated Nanoparticles Loaded with Oxaliplatin

目的:制备叶酸修饰的奥沙利铂纳米粒,对其体外特性进行研究。方法:以载药量、包封率为评价指标,对制备叶酸修饰的奥沙利铂纳米粒的方法(包括薄膜分散法、注入法、超声波分散法、逆向蒸发法)进行筛选,再用正交试验优化制备工艺。结果:采用逆向蒸发法制备叶酸修饰的奥沙利铂纳米粒效果较好,纳米粒的平均粒径为(102±53)nm,Zeta电位为(32.5±5.0)mV,载药量为607.79μg/mL,包封率为82.50%,12 h累积释放量为78.6%。结论:本实验所制备的叶酸修饰的奥沙利铂纳米粒包封率较高、稳定性较好,工艺相对简单,具有良好的应用前景。

Objective：To develop folate-conjugated nanoparticles loaded with oxaliplatin （FA-OHP-NP） and evaluate its release characteristics in vitro. Methods ： The encapsulation rate and drug loading were used to examine in vitro activity of FA-OHP-NP. Firstly, different methods of FA-OHP-NP preparation were performed to screen, including film dispersion method, injection method, ultrasonic dispersion method, reverse evaporation method, then, orthogonal test was conducted to optimize the preparation. Results：It showed that reverse evaporation method was the best candidate for FA-OHP-NP preparation. The average length of this nanoparticles was （ 105 ± 53 ） nm, the Zata potential value was （ 32.5 ± 5.0 ） mv, the drug loading was 607.79μg/mL, the encapsulation rate was 82.5% and the cumulative release for 12 h was 78.6%. Coneluslons：In the study, the encapsulation rate of FA-OHP-NP was high and its preparation process was sim- ple, stability was good. The potential medical applications are exciting.